2,4-Diamino-9H-pyrimido[4,5-b]indol-5-ols: synthesis, in vitro cytotoxic activity, and QSAR investigations
| Autor: | Renate Grünert, Reinhard Troschütz, Jens Landwehr, Patrick J. Bednarski, Bernd Dotzauer, Harald Lanig |
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| Rok vydání: | 2006 |
| Předmět: |
Cisplatin
Indole test Quantitative structure–activity relationship Magnetic Resonance Spectroscopy Spectrophotometry Infrared Chemistry Stereochemistry Alkaloid Organic Chemistry Clinical Biochemistry Pharmaceutical Science Quantitative Structure-Activity Relationship Antineoplastic Agents Biochemistry Chemical synthesis In vitro Mass Spectrometry Pyrimidines Drug Discovery medicine Molecular Medicine Cytotoxic T cell Cytotoxicity Molecular Biology medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry. 14(21) |
| ISSN: | 0968-0896 |
| Popis: | A series of novel 2,4-diaminopyrimido[4,5-b]indol-6-ols has been synthesized and the in vitro cytotoxic activities were evaluated against four human cancer cell lines originating from solid tumors. An increase in activity was observed when a heteroaromatic ring was annulated on side g of the pyrimido[4,5-b]indole system to give compounds with activities comparable to ellipticine and cisplatin. To understand the experimental cytotoxic activities, QSAR investigations were performed, which showed a very good linearity between the experimental and predicted IC(50). |
| Databáze: | OpenAIRE |
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